Search tips
Search criteria 


Logo of aapspharmspringer.comThis journalToc AlertsSubmit OnlineOpen Choice
AAPS PharmSciTech. 2005 June; 6(2): E144–E149.
Published online 2005 September 30. doi:  10.1208/pt060222
PMCID: PMC2750525

Feasibility of transdermal delivery of fluoxetine


Feasibility of developing a transdermal drug delivery of fluoxetine has been investigated. Permeation studies of fluoxetine across human cadaver skin were carried out using Franz diffusion cells. The receptor phase consisted of pH 7.4 phosphate buffer maintained at 37°C. Permeation enhancement of fluoxetine, either in the salt or base form, was achieved using various enhancers like azone, SR-38, and ethanol. Various O/W microemulsion systems of fluoxetine were developed to study their effect on the skin permeation of fluoxetine. The results indicated that ethanol at 65% vol/vol was able to increase the permeation of fluoxetine the most, while microemulsion systems showed decrease in the permeation of fluoxetine. The permeation of fluoxetine obtained using a 65% vol/vol ethanolic solution was found to be sufficient to deliver the required dose (20–80 mg) from a patch of feasible size. The results seem promising for developing a transdermal drug delivery system of fluoxetine.

Keywords: transdermal, fluoxetine, microemulsion, enhancer, ethanol

Full Text

The Full Text of this article is available as a PDF (342K).

Selected References

These references are in PubMed. This may not be the complete list of references from this article.
1. Dreher F, Walde P, Walther P, Wehrli E. Interaction of a lecithin microemulsion gel with human stratum corneum and its effect on transdermal transport. J Control Release. 1997;45:131–140. doi: 10.1016/S0168-3659(96)01559-3. [Cross Ref]
2. Trotta M, Morel S, Gasco MR. Effect of oil phase composition on the skin permeation of felodipine from o/w microemulsions. Pharmazie. 1997;52:50–53. [PubMed]
3. Danielsson I, Lindman B. The definition of microemulsion. Colloid Surf. 1981;3:391–392. doi: 10.1016/0166-6622(81)80064-9. [Cross Ref]
4. Benfield P, Heel RC, Lewis SP. Fluoxetine: review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in depressive illness. Drugs. 1986;32:481–508. doi: 10.2165/00003495-198632060-00002. [PubMed] [Cross Ref]
5. Cold JA, Miller SW, Thomas S, Chow M. Weight loss in an elderly woman receiving fluoxetine. Consultant Pharmacist. 1995;10:97–98.
6. Fichtner CG, Braun BG. Hyperphagia and weight loss during fluoxetine treatment. Ann Pharmacother. 1994;28:1350–1352. [PubMed]
7. Garritty CM. Pharmacotherapy of attention-deficit hyperactivity disorder. Can Pharm. J. 1996;129:36–37.
8. Reynolds JEF. Martindale’s The Extra Pharmacopoeia. 31st ed. London, England: Royal Pharmaceutical Society; 1996.
9. Altamura AC, Moro AR, Percudani M. Clinical pharmacokinetics of fluoxetine. Clin Pharmacokinet. 1994;26:201–214. doi: 10.2165/00003088-199426030-00004. [PubMed] [Cross Ref]
10. Alderman CP, Seshadri P, Ben-Tovim DI. Effects of serotonin reuptake inhibitors on hemostasis. Ann Pharmacother. 1996;30:1232–1234. [PubMed]
11. Ogiso T, Iwaki M, Paku T. Effect of various enhancers on transdermal penetration of indomethacin and urea, and relationship between penetration parameters and enhancement factors. J Pharm Sci. 1995;84:482–488. doi: 10.1002/jps.2600840418. [PubMed] [Cross Ref]
12. Hadgraft J, Walters KA, Hadgraft J. Pharmaceutical Skin Penetration Enhancement. New York, NY: Marcel Dekker Inc; 1993. Azone: mechanisms of action and clinical effect; pp. 175–197.
13. Ghosh TK, Banga AK. Methods of enhancement of transdermal drug delivery: part IIA, chemical permeation enhancers. Pharm Technol. 1993;17:62–62.
14. Gallarate M, Gasco MR, Trotta M, Chetoni P, Saettone MF. Preparation and evaluation in vitro of solutions and o/w microemulsions containing levobunolol as ion-pair. Int J Pharm. 1993;100:219–225. doi: 10.1016/0378-5173(93)90094-V. [Cross Ref]
15. Rajadhyaksha VJ, Sharma K, Pfister WR, Ghosh TK, Pfister WR, Yum S. Transdermal and Topical Drug Delivery Systems. Boca Raton, FL: CRC Press; 1997. Oxazolidinones: a new class of permeation enhancer; pp. 477–509.
16. Hatanaka T, Shimoyama M, Sugibayashi K, Morimoto Y. Effect of vehicle on the skin permeability of drugs: polyethylene glycol 400-water and ethanol-water binary solvents. J Control Release. 1993;23:247–260. doi: 10.1016/0168-3659(93)90006-Q. [Cross Ref]
17. Berner B, Mazzenga GC, Otte JH, Steffens RJ, Juang R, Ebert CD. Ethanol: water mutually enhanced transdermal therapeutic system II: skin permeation of ethanol and nitroglycerin. J Pharm Sci. 1989;78:402–407. doi: 10.1002/jps.2600780512. [PubMed] [Cross Ref]
18. Knutson K, Krill SL, Zhang J. Solvent-mediated alterations of the stratum corneum. J Control Release. 1990;11:93–103. doi: 10.1016/0168-3659(90)90123-B. [Cross Ref]
19. Megrab NA, Williams AC, Barry BW. Oestradiol permeation across human skin, silastic and snake skin membranes: the effects of ethanol/water co-solvent systems. Int J Pharm. 1995;116:101–112. doi: 10.1016/0378-5173(94)00321-U. [Cross Ref]
20. McEvoy GK. AHFS drug information, fluoxetine hydrochloride. Bethesda MD: American Society of Health-System Pharmacists; 2003. pp. 2199–2214.
21. Suwanpidokkul N, Thongnopnua P, Umprayn K. Transdermal delivery of zidovudine (AZT): the effects of vehicles, enhancers, and polymer membranes on permeation across cadaver pig skin. AAPS PharmSciTech. 2004;5:1–8. doi: 10.1208/pt050348. [PMC free article] [PubMed] [Cross Ref]

Articles from AAPS PharmSciTech are provided here courtesy of American Association of Pharmaceutical Scientists